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  1. Phillyrin: an adipose triglyceride lipase inhibitor supported by molecular docking, dynamics simulation, and pharmacological validation
    Zhou C, Yan L, Xu J, Hamezah HS, Wang T, Du F, et al.
    J Mol Model, 2024 Feb 13;30(3):68.
    PMID: 38347278 DOI: 10.1007/s00894-024-05875-7
    CONTEXT: Adipose triglyceride lipase (ATGL), a key enzyme responsible for lipolysis, catalyzes the first step of lipolysis and converts triglycerides to diacylglycerols and free fatty acids (FFA). Our previous work suggested that phillyrin treatment improves insulin resistance in HFD-fed mice, which was associated with ATGL inhibition. In this study, using docking simulation, we explored the binding pose of phillyrin and atglistatin (a mouse ATGL inhibitor) to ATGL in mouse. From the docking results, the interactions with Ser47 and Asp166 were speculated to have caused phillyrin to inhibit ATGL in mice. Further, molecular dynamics simulation of 100 ns and MM-GBSA were conducted for the protein-ligand complex, which indicated that the system was stable and that phillyrin displayed a better affinity to ATGL than did atglistatin throughout the simulation period. Moreover, the results of pharmacological validation were consistent with those of the in silico simulations. In summary, our study illustrates the potential of molecular docking to accurately predict the binding protein produced by AlphaFold and suggests that phillyrin is a potential small molecule that targets and inhibits ATGL enzymatic activity.

    METHODS: The ATGL-predicted protein structure, verified by PROCHECK, was determined using AlphaFold. Molecular docking, molecular dynamics simulation, and prime molecular mechanic-generalized born surface area were performed using LigPrep, Desmond, and prime MM-GBSA modules of Schrödinger software release 2021-2, respectively. For pharmacological validation, immunoblotting was performed to assess ATGL protein expression. The fluorescence intensity and glycerol concentration were quantified to evaluate the efficiency of phillyrin in inhibiting ATGL.

    Matched MeSH terms: Phenylurea Compounds*
  2. Elimination of field colonies of a mound-building termite Globitermes sulphureus (Isoptera: Termitidae) by bistrifluron bait
    Neoh KB, Jalaludin NA, Lee CY
    J Econ Entomol, 2011 Apr;104(2):607-13.
    PMID: 21510212
    The efficacy of Xterm, which contains 1% bistrifluron, in the form of cellulose bait pellets was evaluated for its efficacy in eradicating field colonies of the mound-building termite Globitermes sulphureus (Haviland) (Isoptera: Termitidae). The termite mounds were dissected at the end of the experiment to determine whether the colonies were eliminated. By approximately 2 mo postbaiting, the body of termite workers appeared marble white, and mites were present on the body. The soldier-worker ratio increased drastically in the colonies, and the wall surface of the mounds started to erode. Colony elimination required at least a 4-mo baiting period. Mound dissection revealed wet carton materials (food store) that were greatly consumed and overgrown by fast-growing fungi. Decaying cadavers were scattered all over the nests. On average, 84.1 +/- 16.4 g of bait matrix (68.9 +/- 13.4%, an equivalent of 841 +/- 164 mg of bistrifluron) was consumed in each colony. Moreover, we found that a mere 143 mg of bistrifluron was sufficient to eliminate a colony of C. sulphureus.
    Matched MeSH terms: Phenylurea Compounds*
  3. Evaluation of hexaflumuron for controlling the subterranean termite Coptotermes curvignathus (Isoptera: Rhinotermitidae) in Malaysia
    Sajap AS, Amit S, Welker J
    J Econ Entomol, 2000 Apr;93(2):429-33.
    PMID: 10826196
    Cellulosic bait matrices containing 0.5% hexaflumuron were tested against field colonies of the subterranean termite Coptotermes curvignathus Holmgren in Malaysia. Foraging activities of the termites were first monitored for several months by using survey stakes and wood bundles placed in underground monitoring traps. Infested stakes were replaced with bait devices. Termite workers to act as recruits were collected from infested stakes and placed in the bait devices. Subsequent activities of the termites were monitored by examining and weighing the wood in the monitoring traps. Data show that the four colonies had populations of 166,288-709,052 foragers and mean wood consumption rates of 305.9-508.2 g/mo per trap. These colonies ceased their activities at all monitoring devices 25-44 d after baiting had commenced. Colonies consumed approximately 27-79 g of bait matrix or 137.5-395 mg of hexaflumuron. Thus, C. curvignathus colonies could be monitored, characterized, baited, and foraging eliminated by using a bait matrix containing hexaflumuron.
    Matched MeSH terms: Phenylurea Compounds
  4. Colony Size Affects the Efficacy of Bait Containing Chlorfluazuron Against the Fungus-Growing Termite Macrotermes gilvus (Blattodea: Termitidae)
    Lee CC, Neoh KB, Lee CY
    J Econ Entomol, 2014 12;107(6):2154-62.
    PMID: 26470081 DOI: 10.1603/EC14193
    The efficacy of chitin synthesis inhibitors (CSIs) against fungus-growing termites is known to vary. In this study, 0.1% chlorfluazuron (CFZ) cellulose bait was tested against medium and large field colonies of Macrotermes gilvus (Hagen). The termite mounds were dissected to determine the health of the colony. Individual termites (i.e., workers and larvae) and fungus combs were subjected to gas chromatography-mass spectrometry (GC-MS) analysis to detect the presence of CFZ. In this study, 540.0 ± 25.8 g (or equivalent to 540.0 ± 25.8 mg active ingredient) and 680.0 ± 49.0 g (680.0 ± 49.0 mg active ingredient) of bait matrix were removed by the medium- and large-sized colonies, respectively, after baiting. All treated medium-sized colonies were moribund. The dead termites were scattered in the mound, larvae were absent, population size had decreased by 90%, and the queens appeared unhealthy. In contrast, no or limited effects were found in large-sized colonies. Only trace amounts of CFZ were detected in workers, larvae, and fungus combs, and the population of large-sized colonies had declined by only up to 40%. This might be owing to the presence of large amount of basidiomycete fungus and a drastic decrease of CFZ content per unit fungus comb (a main food source of larvae) in the large-sized colonies, and hence reduced the toxic effect and longer time is required to accumulate the lethal dose in larvae. Nevertheless, we do not deny the possibility of CSI bait eliminating or suppressing the higher termite if the test colonies could pick up adequate lethal dose by installing more bait stations and prolonging the baiting period.
    Matched MeSH terms: Phenylurea Compounds/administration & dosage*
  5. Role of sirtuin 1 (SIRT1) in regulation of autophagy and nuclear factor-kappa Beta (NF-ĸβ) pathways in sorafenib-resistant hepatocellular carcinoma (HCC)
    Chan HY, Ramasamy TS, Chung FF, Teow SY
    Cell Biochem Biophys, 2024 Jun;82(2):959-968.
    PMID: 38466472 DOI: 10.1007/s12013-024-01247-3
    Hepatocellular carcinoma (HCC) remains a major global health problem with high incidence and mortality. Diagnosis of HCC at late stages and tumour heterogeneity in patients with different genetic profiles are known factors that complicate the disease treatment. HCC therapy becomes even more challenging in patients with drug resistance such as resistance to sorafenib, which is a common drug used in HCC patients. Sorafenib resistance can further aggravate HCC by regulating various oncogenic pathways such as autophagy and nuclear factor-kappa Beta (NF-ĸβ) signalling. Sirtuin 1 (SIRT1), is a nicotinamide adenosine dinucleotide (NAD)-dependent histone deacetylases that regulates various metabolic and oncogenic events such as cell survival, apoptosis, autophagy, tumourigenesis, metastasis and drug resistance in various cancers, but its role in HCC, particularly in sorafenib resistance is underexplored. In this study, we generated sorafenib-resistant HepG2 and Huh-7 liver cancer cell models to investigate the role of SIRT1 and its effect on autophagy and nuclear factor-kappa Beta (NF-ĸβ) signalling pathways. Western blot analysis showed increased SIRT1, altered autophagy pathway and activated NF-ĸβ signalling in sorafenib-resistant cells. SIRT1-silenced HCC cells demonstrated down-regulated autophagy in both parental and chemoresistant cells. This may occur through the deacetylation of key autophagy molecules such as FOXO3, beclin 1, ATGs and LC3 by SIRT1, highlighting the role of SIRT1 in autophagy induction. Silencing of SIRT1 also resulted in activated NF-ĸβ signalling. This is because SIRT1 failed to deacetylate p65 subunit of NF-κB, translocate the NF-κB from nucleus to cytoplasm, and suppress NF-κB activity due to the silencing. Hence, the NF-κB transcriptional activity was restored. These findings summarize the role of SIRT1 in autophagy/NF-ĸβ regulatory axis, with a similar trend observed in both parental and sorafenib-resistant cells. The present work promotes a better understanding of the role of SIRT1 in autophagy and NF-ĸβ signalling in HCC and sorafenib-resistant HCC. As some key proteins in these pathways are potential therapeutic targets, a better understanding of SIRT1/autophagy/NF-ĸβ axis could further improve the therapeutic strategies against HCC.
    Matched MeSH terms: Phenylurea Compounds/pharmacology; Phenylurea Compounds/therapeutic use
  6. In vitro and in vivo evaluation of drug-eluting microspheres designed for transarterial chemoembolization therapy
    Wang Y, Molin DG, Sevrin C, Grandfils C, van den Akker NM, Gagliardi M, et al.
    Int J Pharm, 2016 Apr 30;503(1-2):150-62.
    PMID: 26965198 DOI: 10.1016/j.ijpharm.2016.03.002
    Poly(d,l-lactic acid) biodegradable microspheres, loaded with the drugs cisplatin and/or sorafenib tosylate, were prepared, characterized and studied. Degradation of the microspheres, and release of cisplatin and/or sorafenib tosylate from them, were investigated in detail. Incubation of the drug-carrying microspheres in phosphate buffered saline (pH=7.4) revealed slow degradation. Nevertheless, significant release of cisplatin and sorafenib tosylate from microspheres loaded with both drugs was apparent in vitro; this can be attributed to their porous structure. Supernatants from microspheres loaded with both drugs showed strong toxic effects on cells (i.e. endothelial cells, fibroblast cells and Renca tumor cells) and potent anti-angiogenic effect in the matrigel endothelial tube assay. In vivo anti-tumor effects of the microspheres were also observed, in a Renca tumor mouse model. The poly(d,l-lactic acid) microspheres containing both cisplatin and sorafenib tosylate revealed highest therapeutic efficacy, probably demonstrating that combined local administration of cisplatin and sorafenib tosylate synergistically inhibits tumor growth in situ. In conclusion, this study demonstrates the applicability of biodegradable poly(d,l-lactic acid) microspheres loaded with cisplatin and sorafenib tosylate for local drug delivery as well as the potential of these microspheres for future use in transarterial chemoembolization.
    Matched MeSH terms: Phenylurea Compounds
  7. Induction, Subculture Cycle, and Regeneration of Callus in Safed Musli (Chlorophytum borivilianum) using Different Types of Phytohormones
    Nakasha JJ, Sinniah UR, Kemat N, Mallappa KS
    Pharmacogn Mag, 2016 Jul;12(Suppl 4):S460-S464.
    PMID: 27761075
    BACKGROUND: Chlorophytum borivilianum is an industrially valued medicinal crop. Propagation through seeds is not feasible because of low germination percentage and long dormancy period. Therefore, callus culture and plant regeneration can be an alternative to improve this crop production. Also, callus can serve as an alternative source of bioactive compounds.

    OBJECTIVE: To evaluate the effect of different phytohormones on callus induction, subculture cycle, and regeneration studies of callus in C. borivilianum.

    MATERIALS AND METHODS: Young shoot buds of C. borivilianum were inoculated on Murashige and Skoog medium fortified with 3% sucrose and different concentrations (0, 1, 5, 10, and 15 mg/L) of either naphthalene acetic acid or 2,4-dichlorophenoxyacetic acid or indole-3-acetic acid and callus induction was evaluated up to four subcultures cycles. Shoot regeneration from callus was studied on Murashige and Skoog media fortified with 6-benzylaminopurine andkinetin or thidiazuron at varied levels (0, 0.5, 1, 2, and 3 mg/L). Microshoots were rooted on Murashige and Skoog media supplemented with 1.0 mg/L indole-3-butyric acid and plantlets were acclimatized before transferred to the natural conditions.

    RESULTS: Callus induction was better evidenced on Murashige and Skoog media containing 5 mg/L 2,4-dichlorophenoxyacetic acid up to fourth subculture. Callus differentiated into shoots on Murashige and Skoog media fortified with 6-benzylaminopurine or kinetin, whereas thidiazuron completely failed to regenerate shoots. Furthermore, microshoots rooted on 1.0 mg/L indole-3-butyric acid containing Murashige and Skoog media. The rooted plantlets were successfully acclimatized and established in soil with 88.3% survivability.

    CONCLUSION: The type of auxins played an important role in inducing callus tissue from shoot bud explants of Safed musli. In future, this in vitro protocol could benefit in crop improvement programs and serve as a new source of bioactive compounds from Safed musli callus tissue for various therapeutic applications.

    SUMMARY: Explants de-differentiated to form callus on Murashige and Skoog media containing 5 mg/L 2,4-D up to fourth subculture.Callus re-differentiated into shoots on Murashige and Skoog media fortified with 0.5 mg/L BAP.In vitro rooting of shoots was achieved on 1.0 mg/L IBA containing Murashige and Skoog media.The rooted plantlets were successfully acclimatized and established in soil with 88.3% survivability. Abbreviations used: MS: Murashige and Skoog, NAA: naphthalene acetic acid, 2,4-D: 2,4-dichlorophenoxyacetic acid, IAA: indole-3-acetic acid, BAP: 6-benzylaminopurine, Kn: Kinetin, TDZ: thidiazuron, IBA: indole-3-butyric acid, RCBD: Randomized Complete Block Design, DMRT: Duncan's Multiple Range Test.

    Matched MeSH terms: Phenylurea Compounds
  8. Sorafenib in renal cell carcinoma
    Davoudi ET, bin-Noordin MI, Javar HA, Kadivar A, Sabeti B
    Pak J Pharm Sci, 2014 Jan;27(1):203-8.
    PMID: 24374450
    Cancer is among most important causes of death in recent decades. Whoever the renal cell carcinoma incidence is low but it seems it is more complicated than the other cancers in terms of pathophysiology and treatments. The purpose of this work is to provide an overview and also deeper insight to renal cell carcinoma and the steps which have been taken to reach more specific treatment and target therapy, in this type of cancer by developing most effective agents such as Sorafenib. To achieve this goal hundreds of research paper and published work has been overviewed and due to limitation of space in a paper just focus in most important points on renal cell carcinoma, treatment of RCC and clinical development of Sorafenib. The information presented this paper shows the advanced of human knowledge to provide more efficient drug in treatment of some complicated cancer such as RCC in promising much better future to fight killing disease.
    Matched MeSH terms: Phenylurea Compounds/therapeutic use*
  9. Painful Rashes on the Palms and Soles
    Bhullar M, Bhullar A, Arachchi NJ
    Ann Acad Med Singap, 2016 Oct;45(10):479-480.
    PMID: 27832225
    Matched MeSH terms: Phenylurea Compounds/adverse effects*
  10. Statewide Efficacy Assessment of Insect Growth Regulators Against Aedes albopictus (Diptera: Culicidae) in Sabah, Malaysia: An Alternative Control Strategy?
    Elia-Amira NMR, Chen CD, Low VL, Lau KW, Haziqah-Rashid A, Amelia-Yap ZH, et al.
    J Med Entomol, 2022 01 12;59(1):301-307.
    PMID: 34459477 DOI: 10.1093/jme/tjab146
    The efficacy of three groups of insect growth regulators, namely juvenile hormone mimics (methoprene and pyriproxyfen), chitin synthesis inhibitors (diflubenzuron and novaluron), and molting disruptor (cyromazine) was evaluated for the first time, against Aedes albopictus Skuse (Diptera: Culicidae) larvae from 14 districts in Sabah, Malaysia. The results showed that all field populations of Ae. albopictus were susceptible towards methoprene, pyriproxyfen, diflubenzuron, novaluron, and cyromazine, with resistance ratio values ranging from 0.50-0.90, 0.60-1.00, 0.67-1.17, 0.71-1.29, and 0.74-1.07, respectively. Overall, the efficacy assessment of insect growth regulators in this study showed promising outcomes and they could be further explored as an alternative to conventional insecticides.
    Matched MeSH terms: Phenylurea Compounds/pharmacology
  11. Fulltext Multicenter phase II study of sequential radioembolization-sorafenib therapy for inoperable hepatocellular carcinoma
    Chow PK, Poon DY, Khin MW, Singh H, Han HS, Goh AS, et al.
    PLoS One, 2014;9(3):e90909.
    PMID: 24614178 DOI: 10.1371/journal.pone.0090909
    The safety and tolerability of sequential radioembolization-sorafenib therapy is unknown. An open-label, single arm, investigator-initiated Phase II study (NCT0071279) was conducted at four Asia-Pacific centers to evaluate the safety and efficacy of sequential radioembolization-sorafenib in patients with hepatocellular carcinoma (HCC) not amenable to curative therapies.
    Matched MeSH terms: Phenylurea Compounds/adverse effects; Phenylurea Compounds/therapeutic use*
  12. A Case Study on Chronic Hepatitis-C Viral infection Associated with Hepatocellular Carcinoma in a Tertiary Hospital of Bangladesh
    Islam MJ, Saha SK, Das AK, Jahan MS, Pervin S, Karim CF, et al.
    Mymensingh Med J, 2019 Oct;28(4):935-939.
    PMID: 31599264
    Hepatocellular carcinoma (HCC) is an important reason of liver-related death globally. HCC is the fifth most common cancer, the third most common cause for cancer related death in the world and responsible for approximately one million deaths each year. The incidence of HCC is expected to increase in the next two decades, largely due to hepatitis C infection and secondary cirrhosis. We have reported a case of hepatocellular carcinoma in a 56-year-old man with peritoneal metastasis. Diagnostic imaging (Ultra sonogram & CT-Scan) shown: a large hypo density, irregular outline lesion noted in right lower liver, post contrast image shown patchy enhancement of the lesion. His serum Alpha-Feto Protein (AFP) level was very high with elevated serum alanine amino transaminase (ALT) enzyme and prothrombin time. Histopathological (microscopic) features are compatible with Hepatocellular carcinoma. His Hepatitis C viral DNA load e.g., core protein variants and genotype 1, have been reported. The patient was treated by surgical resection followed by conservative treatment includes sorafenib & interferon alpha. This case report aims to outlines the epidemiology of HCC in chronic HCV, risk factors and pathophysiology that contribute to this disease process, related pathophysiology of patient's clinical features, screening recommendations, and the available statistics on the impact of new direct-acting antiviral treatment on the development on HCC.
    Matched MeSH terms: Phenylurea Compounds
  13. Optimization of in vitro regeneration and Agrobacterium tumefaciens-mediated transformation with heat-resistant cDNA in Brassica oleracea subsp. italica cv. Green Marvel
    Ravanfar SA, Aziz MA, Saud HM, Abdullah JO
    Curr Genet, 2015 Nov;61(4):653-63.
    PMID: 25986972 DOI: 10.1007/s00294-015-0494-x
    An efficient system for shoot regeneration and Agrobacterium tumefaciens-mediated transformation of Brassica oleracea cv. Green Marvel cultivar is described. This study focuses on developing shoot regeneration from hypocotyl explants of broccoli cv. Green Marvel using thidiazuron (TDZ), zeatin, and kinetin, the optimization of factors affecting Agrobacterium-mediated transformation of the hypocotyl explants with heat-resistant cDNA, followed by the confirmation of transgenicity of the regenerants. High shoot regeneration was observed in 0.05-0.1 mg dm(-3) TDZ. TDZ at 0.1 mg dm(-3) produced among the highest percentage of shoot regeneration (96.67 %) and mean number of shoot formation (6.17). The highest percentage (13.33 %) and mean number (0.17) of putative transformant production were on hypocotyl explants subjected to preculture on shoot regeneration medium (SRM) with 200 µM acetosyringone. On optimization of bacterial density and inoculation time, the highest percentage and mean number of putative transformant production were on hypocotyl explants inoculated with a bacterial dilution of 1:5 for 30 min. Polymerase chain reaction (PCR) assay indicated a transformation efficiency of 8.33 %. The luciferase assay showed stable integration of the Arabidopsis thaliana HSP101 (AtHSP101) cDNA in the transgenic broccoli regenerants. Three out of five transgenic lines confirmed through PCR showed positive hybridization bands of the AtHSP101 cDNA through Southern blot analysis. The presence of AtHSP101 transcripts in the three transgenic broccoli lines indicated by reverse transcription-PCR (RT-PCR) confirmed the expression of the gene. In conclusion, an improved regeneration system has been established from hypocotyl explants of broccoli followed by successful transformation with AtHSP101 for resistance to high temperature.
    Matched MeSH terms: Phenylurea Compounds/pharmacology
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